Honoring our heritage and moving ahead

Nóbrega, Joaquim A.; Hatje, Vanessa

doi:10.1590/s0103-50532013000100001

Cited by 2 publications

(1 citation statement)

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“…[6][7][8][9][10][11][12][13] Embora não faça parte do escopo do Journal of the Brazilian Chemical Society da SBQ, que divulga os trabalhos de pesquisa em inglês, o periódico tem contribuído com a discussão da pós-graduação em química no país por meio de seus editoriais. [14][15][16] Visando uma melhor comunicação e transparência, a CAPES criou uma página para cada área de avaliação, na qual estão acessíveis os documentos de área e relatório de avalição desde a Trienal 2010, critérios para submissão de novas propostas (APCN), atualizações e critérios qualis e seminários de acompanhamento. 17 Embora várias informações sobre os programas da área estejam disponibilizadas pela CAPES, nesse artigo pretende-se abordar a evolução e o estado da arte dos programas de pós-graduação da área de Química e o seu papel na formação de recursos humanos qualificados, indispensáveis para o desenvolvimento sustentável do país.…”

Section: Introductionunclassified

Sistema Nacional de Pós-Graduação e a Área de Química na CAPES

2017

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Section: Introductionunclassified

Sistema Nacional de Pós-Graduação e a Área de Química na CAPES

2017

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Synthesis of New Thiosemicarbazones and Semicarbazones Containing the 1,2,3-1H-triazole-isatin Scaffold: Trypanocidal, Cytotoxicity, Electrochemical Assays, and Molecular Docking

Silva

Sales

Romanha

et al. 2019

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Background: Chagas disease, also known as American trypanosomiasis, is classified as one of the 17 most important neglected diseases by the World Health Organization. The only drugs with proven efficacy against Chagas disease are benznidazole and nifurtimox, however both show adverse effects, poor clinical efficacy, and development of resistance. For these reasons, the search for new effective chemical entities is a challenge to research groups and the pharmaceutical industry. Objective: Synthesis and evaluation of antitrypanosomal activities of a series of thiosemicarbazones and semicarbazones containing 1,2,3-1H triazole isatin scaffold. Method: 5&'-(4-alkyl/aryl)-1H-1,2,3-triazole-isatins were prepared by Huisgen 1,3-dipolar cycloaddition and the thiosemicarbazones and semicarbazones were obtained by the 1:1 reactions of the carbonylated derivatives with thiosemicarbazide and semicarbazide hydrochloride, respectively, in methanol, using conventional reflux or microwave heating. The compounds were assayed for in vitro trypanocidal activity against Trypanosoma cruzi, the aetiological agent of Chagas disease. Beyond the thio/semicarbazone derivatives, isatin and triazole synthetic intermediates were also evaluated for comparison. Results: A series of compounds were prepared in good yields. Among the 37 compounds evaluated, 18 were found to be active, in particular thiosemicarbazones containing a non-polar saturated alkyl chain (IC50 = 24.1, 38.6, and 83.2 &µM; SI = 11.6, 11.8, and 14.0, respectively). To further elucidate the mechanism of action of these new compounds, the redox behaviour of some active and inactive derivatives was studied by cyclic voltammetry. Molecular docking studies were also performed in two validated protein targets of Trypanosoma cruzi, i.e., cruzipain (CRZ) and phosphodiesterase C (TcrPDEC). Conclusion: A class of thio/semicarbazones structurally simple and easily accessible was synthesized. Compounds containing thiosemicarbazone moieties showed the best results in the series, being more active than the corresponding semicarbazones. Our results indicated that the activity of these compounds does not originate from an oxidation-reduction pathway but probably from the interactions with trypanosomal enzymes.

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Honoring our heritage and moving ahead

Cited by 2 publications

References 4 publications

Sistema Nacional de Pós-Graduação e a Área de Química na CAPES

Sistema Nacional de Pós-Graduação e a Área de Química na CAPES

Synthesis of New Thiosemicarbazones and Semicarbazones Containing the 1,2,3-1H-triazole-isatin Scaffold: Trypanocidal, Cytotoxicity, Electrochemical Assays, and Molecular Docking

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